GenFleet Therapeutics and Innovent Biologics announced that the first patient with KRAS G12C mutation has been dosed in the first-in-human trial of GFH925 (ClinicalTrials.gov, NCT05005234). Designed to enroll over 100 patients with late stage NSCLC and gastrointestinal cancer, the study will evaluate the safety/tolerability/efficacy and characterize the pharmacokinetics profile of GFH925 administered orally to patients with KRAS G12C mutation. Moreover, this study will explore the potential mechanisms of primary and acquired resistance to KRAS inhibitors. Based on emerging data of GFH925 and other KRAS inhibitors including biomarkers, investigators will look to further optimize the precision treatment plans and the potential for combination therapies. About GFH925:- Being developed by GenFleet Therapeutics, GFH925 is a novel, orally active, potent KRAS G12C inhibitor designed to effectively target the GTP/GDP exchange, an essential step in pathway activation, by modifying the cysteine residue of KRAS G12C protein covalently and irreversibly. Preclinical cysteine selectivity studies demonstrated high selectivity of GFH925 towards G12C. Subsequently, GFH925 effectively inhibits the downstream signal pathway to induce tumor cells' apoptosis and cell cycle arrest. GenFleet Therapeutics and Innovent Biologics entered into an exclusive license agreement in early September for the development and commercialization of GenFleet's lead KRAS G12C candidate, GFH925 in China, including the Chinese mainland, Hong Kong, Macau and Taiwan with additional option-in rights for global development and commercialization.